Hantzsch合成法和氰基缩合法制备Boc-甘氨酸噻唑乙酯比较  

Hantzsch Synthesis and Cyanocondensation for Preparation of Boc-Glycine Thiazole Ethyl Ester

作　　者：任德豪 赵湲湲 高庆英 伊海晨 罗涛 刘义 Ren Dehao;Zhao Yuanyuan;Gao Qingying;Yi Haichen;Luo Tao;Liu Yi(School of Chemical and Chemical Engineering,Yantai University,Yantai 264006,China)

机构地区：[1]烟台大学化学化工学院,山东烟台264006

出　　处：《山东化工》2023年第16期28-31,共4页Shandong Chemical Industry

基　　金：山东省自然科学基金面上项目:ZR2020MB105;烟台大学大学生创新创业训练计划项目。

摘　　要：Boc-甘氨酸噻唑乙酯是一种重要的药物合成中间体,是构建天然抗癌药物分子largazole和众多其他药物分子的重要前体。以市售Boc-甘氨酸为原料,分别通过酰胺化、Lawesson硫代、Hantzsch噻唑环化合成路线和经过酰胺化、氰基化、缩合反应的合成路线,完成了Boc-甘氨酸噻唑乙酯的制备和结构表征。从合成产率、后处理复杂程度、可操作性等方面,对两条合成路线进行了系统对比和分析。Boc-glycine thiazole ethyl ester is an important intermediate for drug synthesis.It is also an important precursor for the construction of largazole,a natural anticancer drug molecule,and numerous other drug molecules.In this thesis,using commercially available Boc-glycine as starting material,the Boc-glycine thiazole ethyl ester was respectively synthesized via two synthetic routes.One synthetic route was constructed by amidation/Lawesson reaction/Hantzsch thiazole cyclization,and the other synthetic route was constructed by amidation/cyanidation/condensation reactions for the preparation and structural characterization of Boc-glycine thiazole ethyl esters.The paper systematically compares and analysizes two synthetic routes in terms of synthetic yield,post-treatment complexity and operability.

关 键 词：噻唑 Hantzsch合成法 药物中间体 路线比较 

分 类 号：O621.3[理学—有机化学] O69[理学—化学]